Development, characterization and anti - Mycobacterium tuberculosis activity of solid lipid nanoparticles for oral Piper corcovadensis roots extract delivery / Desarrollo, caracterización y actividad anti - Mycobacterium tuberculosis de nanopartículas lipídicas sólidas para la administración oral de extracto de raíces de Piper corcovadensis

The present study thus aimed at the development and physicochemical characterization of solid lipid nanoparticles loaded with crude extract of Piper corcovadensis roots (SLN - CEPc) and chitosan - coated solid lipid nanoparticles loaded with crude extract of P. corcovadensis roots (C - SLN - CEPc), as well as the determination of its antimycobacterial activity against Mycobacterium tuberculosis H37Rv, its cytotoxicity against the Vero cell line and evaluation in the hemolysis assay. Both formulat ions containing the encapsulated extract showed high encapsulation efficiency, formed by a monodispersed system with small and spherical particles, and there was no aggregation of particles. In the biological assays, SLN - CEPc and C - SLN - CEPc showed promisin g anti - M. tuberculosis activity with a minimum inhibitory concentration (MIC) of 12.5 µg/mL, whereas the cytotoxic concentrations obtained at 50% (CC 50 ) in Vero cells were 60.0 and 70.0 µg/mL, respectively. Therefore, nanoencapsulation showed satisfactory results, justifying its usage in the development of new products.

El presente estudio apuntó al desarrollo y caracterización fisicoquímica de na nopartículas lípidas en estado sólido, cargadas con extracto crudo de raíz de Piper c orcovadensis (SLN - CEPc) y nanopartículas lípidas en estado sólido cubiertas con quitosano cargadas co n extracto crudo de raíz de P. corcovadensis (C - SLN - CEPc), así como la determinación de su actividad antimico bacterial contra Mycobacterium tuberculosis H37Rv, su citotoxicidad contra la línea celular Vero y su evaluación en ensayo de hemólisis. Ambas formulaciones que contenían el extracto encapsulado mostraron alta eficien cia de encapsulación, formado por un sistema monodispersado con pequeñas partículas esféricas, y no hubo agregación de partículas. En los ensayos biológicos, SLN - CEPc y C - SLN - CEPc mostraron un a prometedora actividad anti - M. tuberculosis con una mínima conc entración inhibitoria (MIC) de 12,5 µg/mL, mientras que las concentraciones citotóxicas obtenidas al 50% (CC 50 ) en células Vero estuvo en 60,0 y 70,0 µg/mL, respectivamente. Por lo tanto, la nanoencapsulación mostró resultados satisfactorios, justificando su uso en el desarrollo de nuevos productos.

Lutein-loaded nanoparticles reverse oxidative stress, apoptosis, and autism spectrum disorder-like behaviors induced by prenatal valproic acid exposure in female rats.

Autism spectrum disorder (ASD) is a neurodevelopmental disorder characterized by deficits in social interaction and repetitive behaviors. In this study, we assessed the effect of lutein-loaded nanoparticles on ASD-like behaviors induced by prenatal valproic acid (VPA) exposure in female offspring rats and the possible involvement of oxidative stress and apoptosis. Pregnant female Wistar rats received a single intraperitoneal injection of VPA (600 mg/kg), on the gestational day 12.5. The VPA-exposed female offspring rats were divided into two subgroups and received either lutein-loaded nanoparticles (5 mg/kg) or saline by oral gavage, for 14 days. The animals were submitted to the three-chamber test and open field to evaluate ASD-like behaviors. The hippocampus was removed for the determination of oxidative stress indicators (ROS; TBARS; SOD and Nrf2) and apoptosis biomarkers (Hsp-70; p38-MAPK; Bax and Bcl-2). The exposure to lutein-loaded nanoparticles reversed sociability deficit, social memory deficit, and anxiety-like and repetitive behaviors induced by VPA, and restored the oxidative stress indicators and apoptosis biomarkers in the hippocampus. This neurochemical effect must be associated with the reversal of ASD-like behaviors. These results provide evidence that lutein-loaded nanoparticles are an alternative treatment for VPA-induced behavioral damage in female rats and suggest the involvement of oxidative stress.